CPI-613

CPI-613 is a lipoic acid analog that inhibits α-ketoglutarate dehydrogenase, particularly in tumor cells.¹ At 60-240 µM, CPI-613 induces a strong mitochondrial burst of reactive oxygen species, resulting in cell death.¹ By disrupting mitochondrial metabolism, CPI-613 demonstrates both in vitro and in vivo anti-tumor activity through both apoptotic and non-apoptotic pathways.^2,3,4

WARNING This product is not for human or veterinary use.

1. Stuart, S.D., Schauble, A., Gupta, S., et al. A strategically designed small molecule attacks alpha-ketoglutarate dehydrogenase in tumor cells through a redox process. Cancer Metab. 2(1), 4 (2014).

2. Lee, K.C., Shorr, R., Rodriguez, R., et al. Formation and anti-tumor activity of uncommon in vitro and in vivo metabolites of CPI-613, a novel anti-tumor compound that selectively alters tumor energy metabolism. Drug Metab. Lett. 5(3), 163-182 (2011).

3. Zachar, Z., Marecek, J., Maturo, C., et al. Non-redox-active lipoate derivates disrupt cancer cell mitochondrial metabolism and are potent anticancer agents in vivo. J. Mol. Med. (Berl.) 89(11), 1137-1148 (2011).

4. Lee, K.C., Maturo, C., Perera, C.N., et al. Translational assessment of mitochondrial dysfunction of pancreatic cancer from in vitro gene microarray and animal efficacy studies, to early clinical studies, via the novel tumor-specific anti-mitochondrial agent, CPI-613. Ann. Transl. Med. 2(9), 91 (2014).